Synthesis and in vitro antifungal activities of new 3-substituted benzopyrone derivatives

被引：13

作者：

Lv, Zhiliang ^{[1
]}

Sheng, Chunquan ^{[1
]}

Zhang, Yikai ^{[1
]}

Wang, Tiantian ^{[1
]}

Feng, Jilu ^{[1
]}

Sun, Hailing ^{[1
]}

Zhong, Hanyu ^{[1
]}

Zhang, Mingfeng ^{[1
]}

Chen, Huan ^{[1
]}

Li, Ke ^{[1
]}

机构：

[1] Second Mil Med Univ, Sch Pharm, Dept Med Chem, Shanghai 200433, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 23期

基金：

中国国家自然科学基金;

关键词：

Antifungal activity; Benzopyrone derivative; Synthesis; Lanosterol 14 alpha-demethylase (CYP51); Molecular docking; LANOSTEROL; 14-ALPHA-DEMETHYLASE; FLUCONAZOLE; DESIGN; AZOLES;

D O I：

10.1016/j.bmcl.2010.09.072

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of new benzopyrone compounds were designed and synthesized and their antifungal activities in vitro were evaluated. The results showed that the benzopyrone derivatives with short terminal alkyl chain exhibited potent antifungal activity, which represent a novel class of promising leads for the development of novel non-azole antifungal agents. Compound 5j is the most potent one with MIC80 value 1.5 mu g/mL against Trichophyton rubrum. Flexible molecular docking was used to analyze the structure-activity relationships (SARs) of the compounds. The designed compounds interact with CA-CYP51 through hydrophobic and van der Waals interactions. Crown Copyright (C) 2010 Published by Elsevier Ltd. All rights reserved.

引用

页码：7106 / 7109

页数：4

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